# US 8,541,425 B2 · Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors

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- Number: US 8,541,425 B2
- Document ID: US8541425B2
- Status: Granted
- Kind: B2
- Application number: 12/549,170
- Filed: 2009-08-27
- Published: 2010-01-28
- Granted: 2013-09-24
- Earliest claimed: 2005-12-13
- Assignees: Incyte Corporation
- Applicants: James D. Rodgers; Stacey Shepard; Jordan S. Fridman; Krishna Vaddi
- Inventors: James D. Rodgers; Stacey Shepard; Jordan S. Fridman; Krishna Vaddi
- Web page: https://patentgrep.com/patent/US8541425B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 17/04: Antipruritics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/12: Antivirals
- A61P 35/04: specific for metastasis
- A61P 37/00: Drugs for immunological or allergic disorders
- C07B 59/002: {Heterocyclic compounds}
- C07D 417/04: directly linked by a ring-member-to-ring-member bond
- C07D 471/04: Ortho-condensed systems
- C07D 487/04: Ortho-condensed systems
- C07B 2200/05: Isotopically modified compounds, e.g. labelled
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

## Claims

### Claim 1

A method of treating a disease in a patient, wherein said disease is selected from cachexia, acute myelogenous leukemia, acute lymphoblastic leukemia, and chronic myelomonocytic leukemia, comprising administering to said patient a therapeutically effective amount of a compound which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, wherein said treating refers to ameliorating or inhibiting the disease in the patient.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said compound is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 2)

The method according to claim 2, wherein said disease is acute myelogenous leukemia.

### Claim 4 (depends on 2)

The method according to claim 2, wherein said disease is chronic myelomonocytic leukemia.

### Claim 5 (depends on 2)

The method according to claim 2, wherein said disease is cachexia.

### Claim 6 (depends on 5)

The method according to claim 5, wherein said cachexia results from or is associated with cancer.

### Claim 7 (depends on 2)

The method according to claim 2, wherein said disease is acute lymphoblastic leukemia.